Small molecule anticancer agents drugs

The overexpression of GSTs in some cancer cells, particularly of GST Pl-1, offers an opportunity to detect and treat some cancer types (e.g., ovarian cancer). Recent developments in the design of small molecules that either inhibit the catalytic activity of GST Pl-1 or use GST Pl-1 catalytic site to release the actual anticancer agent, have shown promising results in preclinical studies, with the graduation of 66 and 96 as potential anticancer drug candidates currently undergoing clinical trials. 

Kerr, J. S., Slee, A. M., and Mousa, S. A. Small molecule alpha(v) integrin antagonists Novel anticancer agents. Exp. Opin. Invest. Drugs 9 1271-1279, 2000. 

Buolamwini JK, Addo J, Kamath S, Patil S, Mason D, Ores M. Small molecule antagonists of the MDM2 oncoprotein as anticancer agents. Curr Cancer Drug Targets 2005 5 57-68. 

PEGylated drugs include conjugation with enzymes, peptides, proteins, antibodies, oligonucleotides, anticancer agents and small organic molecules [317]. 

The use of organometallic medicinals is also widespread. Just as small molecules such as cisplatin, the most widely used anticancer drug, are important agents to fight disease, polymeric analogs have been synthesized that exhibit greater specificity, lower toxicities, and increased activity because of their polymeric nature. 

Mas-Moruno C, Rechenmacher F, Kessler H (2010) Cilengitide the first anti-angiogenic small molecule drug candidate. Design, synthesis and clinical evaluation. Anticancer Agents Med Chem 10 753-768... 

---